INTRODUCTIONDendritic cells (DCs) play a key regulatory role inantitumor immunity,especially in its immuneaccessory role via MHC-Ⅰ molecules.We haverecently reported that DCs were able to enhance thekilling activity ...INTRODUCTIONDendritic cells (DCs) play a key regulatory role inantitumor immunity,especially in its immuneaccessory role via MHC-Ⅰ molecules.We haverecently reported that DCs were able to enhance thekilling activity of Lymphokine and PHA activatedkiller (LPAK) cells in vitro.In the presentstudy,we evaluated the effects of GM-CSF andTNF upon antitumor activities of freshly展开更多
Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphyl...Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.展开更多
Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyc...Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization.Then the reaction of substituted coumarins(a-e)with potassium O-ethyl/methyl carbonodithioate(1)by using absolute ethanol as solvent,afforded coumarin-carbonodithioate(1a-1j)derivatives under microwave irradiation and the conventional method.The spectroscopic analysis was used for the characterization of coumarin derivatives.The title(1a-1j)compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard.Drug-likeness.In-silico toxicity was predicted with LD_(50)value and bioactivity score was also calculated for all the compounds.Results:All coumarin(1a-1j)compounds exhibited promisingin-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs.All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule.It was observed that the synthesized compounds followed rule of five,indicating more'drug-like'nature.Conclusions:All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities.From the physicochemical properties of coumarin derivatives,it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five.It is concluded that the coumarin-carbonodithioate hybrids act with more'drug-like'nature.展开更多
基金Natural Science Foundation of the Higher Education Office of Guangdong Province,No.19952901
文摘INTRODUCTIONDendritic cells (DCs) play a key regulatory role inantitumor immunity,especially in its immuneaccessory role via MHC-Ⅰ molecules.We haverecently reported that DCs were able to enhance thekilling activity of Lymphokine and PHA activatedkiller (LPAK) cells in vitro.In the presentstudy,we evaluated the effects of GM-CSF andTNF upon antitumor activities of freshly
文摘Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.
文摘Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization.Then the reaction of substituted coumarins(a-e)with potassium O-ethyl/methyl carbonodithioate(1)by using absolute ethanol as solvent,afforded coumarin-carbonodithioate(1a-1j)derivatives under microwave irradiation and the conventional method.The spectroscopic analysis was used for the characterization of coumarin derivatives.The title(1a-1j)compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard.Drug-likeness.In-silico toxicity was predicted with LD_(50)value and bioactivity score was also calculated for all the compounds.Results:All coumarin(1a-1j)compounds exhibited promisingin-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs.All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule.It was observed that the synthesized compounds followed rule of five,indicating more'drug-like'nature.Conclusions:All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities.From the physicochemical properties of coumarin derivatives,it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five.It is concluded that the coumarin-carbonodithioate hybrids act with more'drug-like'nature.
文摘目的:研究芦荟多糖的提取、纯化工艺及体外抗肿瘤活性,为芦荟的产业化开发提供实验依据。方法:采用水提醇沉,三氯乙酸法除蛋白,DEAE-52离子交换色谱分离。用Sephacryl S-400凝胶柱层析纯化并确定芦荟多糖的相对分子量,HPLC法检测纯度,GC法鉴别单糖组成及分子摩尔比。以MTT法观察其体外抗肿瘤活性等。结果:从中华芦荟(Aloe vera L.var. chinesis(Haw.)Berger.)凝胶冻干粉中提取分离得到纯多糖AVP,经HPLC检测为单一对称峰,相对分子量为86000,由甘露糖和葡萄糖组成,摩尔比为10.3∶1.0。AVP对人肝癌细胞(SMMC-7721)、人胃癌细胞(BGC-823)及人肺癌细胞(A549)的增殖均有抑制作用。结论:该法分离的芦荟多糖AVP纯度好,收率高达3.6%,可用于进一步的研究和开发,提高芦荟的资源利用率。
